This application is a 371 of PCT/EP99/00184, filed Jan. 14, 1999
The present invention relates to a novel method of controlling pests in and on transgenic crops of useful plants with pymetrozine; profenofos; a benzoylurea-derivative, especially lufenuron; or a carbamat-derivative, especially fenoxycarb.
Certain pest control methods are proposed in the literature. However, these methods are not fully satisfactory in the field of pest control, which is why there is a demand for providing further methods for controlling and combating pests, in particular insects and repre-sentatives of the order Acarina, or for protecting plants, especially crop plants. This object is achieved according to the invention by providing the present method.
The present invention therefore relates to a method of controlling pests in crops of transgenic useful plants, such as, for example, in crops of maize, cereals, soya beans, tomatoes, cotton, potatoes, rice and mustard, characterized in that a pesticidal composition comprising pymetrozine; profenofos; a benzoylurea-derivative, especially lufenuron; or a carbamat-derivative, especially fenoxycarb, in free form or in agrochemically useful salt form and at least one auxiliary is applied to the pests or their environment, in particular to the crop plant itself; to the use of the composition in question and to propagation material of transgenic plants which has been treated with it.
Surprisingly, it has now emerged that the use of pymetrozine; profenofos; a benzoylurea-derivative, especially lufenuraon; or a carbamat-derivative, especially fenoxycarb, for controlling pests on transgenic useful plants which containxe2x80x94for instancexe2x80x94one or more genes expressing a pesticidally, particularly insecticidally, acaricidally, nematocidally or fugicidally active ingredient, or which are tolerant against herbicides or resistent against the attack of fungi, has a synergistic effect. It is highly surprising that the use of pymetrozine; profenofos; a benzoylurea-derivative, or a carbamat-derivative in combination with a transgenic plant exceeds the additive effect, to be expected in principle, on the pests to be controlled and thus extends the range of action of the said active ingredients and of the active principle expressed by the transgenic plant in particular in two respects:
In particular, it has been found, surprisingly, that within the scope of invention the pesticidal activity of a active ingredient according to the invention in combination with the effect expressed by the transgenic useful plant, is not only additive in comparison with the pesticidal activities of the active ingredient according to the invention alone and of the transgenic crop plant alone, as can generally be expected, but that a synergistic effect is present. The term xe2x80x9csynergisticxe2x80x9d, however, is in no way to be understood in this connection as being restricted to the pesticidal activity, but the term also refers to other advantageous properties of the method according to the invention compared with the active ingredient according to the invention and the transgenic useful plant alone. Examples of such advantageous properties which may be mentioned are: extension of the pesticidal spectrum of action to other pests, for example to resistant strains; reduction in the application rate of the active ingredient according to the invention, or sufficient control of the pests with the aid of the compositions according to the invention even at an application rate of the active ingredient according to the invention alone and the transgenic useful plant alone are entirely ineffective; enhanced crop safety; improved quality of produce such as higher content of nutrient or oil, better fiber quality, enhanced shelf life, reduced content of toxic products such as mycotoxins, reduced content of residues or unfavorable constituents of any kind or better digestability; improved tolerance to unfavorable temperatures, draughts or salt content of water; enhanced assimilation rates such as nutrient uptake, water uptake and photosynthesis; favorable crop properties such as altered leaf aerea, reduced vegetative growth, increased yields, favorable seed shape/seed thickness or germination properties, altered colonialisation by saprophytes or epiphytes, reduction of senescense, improved phytoalexin production, improved of accelerated ripening, flower set increase, reduced boll fall and shattering, better attraction to beneficials and predators, increased pollination, reduced attraction to birds; or other advantages known to those skilled in the art. pymetrozine, 2,3,4,5-Tetrahydro-3-oxo-4-[(pyridin-3-yl)-methylenamino]-6-methyl-1,2,4-triazin, is known from The Pesticide Manual, 10thEd. (1994), The British Crop Protection Council, London, page 868.
The active ingredients used according to the invention are know to those skilled in the art, specifically:
Carbamates are known for instance from EP-A-004334. Fenoxycarb, Ethyl 2-(4-Phenoxyphenoxy)ethylcarbamat, is known from The Pesticide Manual, 9thEd. (1991), The British Crop Protection Council, London, page 375;
Benzoylureas are known for instance from EP-A-179022; lufenuron is known from The Pesticide Manual, 10thEd. (1994), The British Crop Protection Council, London, page 628; and
Profenofos, O-4-Brom-2-chlorphenyl O-Ethyl S-Propyl Phosphorothioat, is known from The Pesticide Manual, 9thEd. (1991), The British Crop Protection Council, London, page 705.
The agrochemically compatible salts of the active ingredients according to the invention are, for example, acid addition salts of inorganic and organic acids, in particular of hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, perchloric acid, phosphoric acid, formic acid, acetic acid, trifluoroacetic acid, oxalic acid, malonic acid, toluenesulfonic acid or benzoic acid. Preferred within the scope of the present invention is a composition known per se which comprises, as active ingredient, pymetrozine, profenofos, lufenuron or fenoxacarb; each in the free form.
The transgenic plants used according to the invention are plants, or propagation material thereof, which are transformed by means of recombinant DNA technology in such a way that they arexe2x80x94for instancexe2x80x94capable of synthesizing selectively acting toxins as are known, for example, from toxin-producinginvertebrates, especially of the phylum Arthropoda, as can be obtained from Bacillus thuringiensis strains; or as are known from plants, such as lectins; or in the alternative capable of expressing a herbicidal or fungicidal resistance. Examples of such toxins, or transgenic plants which are capable of synthesizing such toxins, have been disclosed, for example, in EP-A-0 374 753, WO 93/07278, WO 95/34656, EP-A-0 427 529 and EP-A-451 878 and are incorporated by reference in the present application.
The methods for generating such transgenic plants are widely known to those skilled in the art and described, for example, in the publications mentioned above.
The toxins which can be expressed by such transgenic plants include, for example, toxins, such as proteins which have insecticidal properties and which are expressed by transgenic plants, for example Bacillus cereus proteins or Bacillus popliae proteins; or Bacillus thuringiensis endotoxins (B.t.), such as CryIA(a), CryIA(b), CryIA(c), CryIIA, CryIIIA, CryIIIB2 or CytA; VIP1; VIP2; VIP3; or insecticidal proteins of bacteria colonising nematodes like Photorhabdus spp or Xenorhabdus spp such as Photorhabdus luminescens, Xenorhabdus nematophilus etc.; proteinase inhibitors, such as trypsin inhibitors, serine protease inhibitors, patatin, cystatin, papain inhibitors; ribosome-inactivating proteins (RIP), such as ricin, maize RIP, abrin, luffin, saporin or bryodin; plant lectins such as pea lectins, barley lectins or snowdrop lectins; or agglutinins; toxins produced by animals, such as scorpion toxins, spider venoms, wasp venoms and other insect-specific neurotoxins; steroid metabolism enzymes, such as 3-hydroxysteroid oxidase, ecdysteroid UDP-glycosyl transferase, cholesterol oxidases, ecdysone inhibitors, HMG-COAreductase, ion channel blockers such as sodium and calcium, juvenile hormone esterase, diuretic hormone receptors, stilbene synthase, bibenzyl synthase, chitinases and glucanases.
Examples of known transgenic plants which comprise one or more genes which encode insecticidal resistance and express one or more toxins are the following: KnockOut(copyright) (maize), YieldGard(copyright) (maize); NuCOTN 33B(copyright) (cotton), Boligard(copyright) (cotton), NewLeaf(copyright) (potatoes), NatureGard(copyright) and Protecta(copyright).
The following tables comprise further examples of targets and principles and crop phenotypes of transgenic crops which show tolerance against pests mainly insects, mites, nematodes, virus, bacteria and diseases or are tolerant to specific herbicides or classes of herbicides.
The abovementioned animal pests which can be controlled by the method according to the invention include , for example, insects, representatives of the order acarina and representatives of the class nematoda; especially
from the order Lepidoptera Acleris spp., Adoxophyes spp., especially Adoxophyes reticulana; Aegeria spp., Agrotis spp., especially Agrotis spinifera; Alabama argiliaceae, Amylois spp., Anticarsia gemmatalis, Archips spp., Argyrotaenia spp., Autographa spp., Busseola fusca, Cadra cautella, Carposina nipponensis, Chilo spp., Choristoneura spp., Clysia ambiguella, Cnaphalocrocis spp., Cnephasia spp., Cochylis spp., Coleophora spp., Crocidolomia binotalis, Cryptophlebia leucotreta, Cydia spp., especially Cydia pomonella; Diatraea spp., Diparopsis castanea, Earias spp., Ephestia spp., especially E. Khxc3xcniella; Eucosma spp., Eupoecilia ambiguella, Euproctis spp., Euxoa spp, Grapholita spp., Hedya nubiferana, Heliothis spp., especially H. Virescens und H. zea; Hellula undalis, Hyphantria cunea, Keiferia lycopersicella, Leucoptera scitella, Lithocollethis spp., Lobesiaspp, Lymantria spp., Lyonetia spp., Malacosoma spp., Mamestra brassicae, Manduca sexta, Operophtera spp., Ostrinia nubilalis, Pammene spp., Pandemis spp., Panolis flammea, Pectinophora spp., Phthorimaea operculella, Pieris rapae, Pieris spp., Plutella xylostella, Prays spp., Scirpophaga spp., Sesamia spp., Sparganothis spp., Spodopteralittoralis, Synanthedon spp., Thaumetopoea spp., Tortrix spp., Trichoplusia ni and Yponomeuta spp.; from the order Coleoptera, for example Agriotes spp., Anthonomus spp., Atomaria linearis, Chaetocnema tibialis, Cosmopolites spp., Curculio spp., Dermestes spp., Diabrotica spp., Epilachna spp., Eremnus spp., Leptinotarsa decemlineata, Lissorhoptrus spp., Melolontha spp., Oryzaephilus spp., Otiorhynchus spp., Phlyctinus spp., Popillia spp., Psylliodes spp., Rhizopertha spp., Scarabeidae, Sitophilus spp., Sitotroga spp., Tenebrio spp., Tribolium spp. and Trogoderma spp.;
from the order Orthoptera, for example Blatta spp., Blattella spp., Gryllotalpa spp., Leucophaea maderae, Locusta spp., Periplaneta spp. and Schistocerca spp.;
from the order Isoptera, for example Reticulitermes spp.;
from the order Psocoptera, for example Liposcelis spp.;
from the order Anoplura, for example Haematopinus spp., Linognathus spp., Pediculus spp., Pemphigus spp. and Phylloxera spp.;
from the order Mallophaga, for example Damalinea spp. and Trichodectes spp.;
from the order Thysanoptera, for example Frankliniella spp., Hercinothrips spp., Taeniothrips spp., Thrips palmi, Thrips tabaci and Scirtothrips aurantii; 
from the order Heteroptera, for example Cimex spp., Distantiella theobroma, Dysdercus spp., Euchistus spp. Eurygaster spp. Leptocorisa spp., Nezara spp., Piesma spp., Rhodnius spp., Sahlbergella singularis, Scotinophara spp. and Triatoma spp.; from the order Homoptera, for example Aleurothrixus floccosus, Aleyrodes brassicae, Aonidiella aurantii, Aphididae, Aphis craccivora, A. fabae, A. gosypii; Aspidiotus spp., Bemisia tabaci, Ceroplaster spp., Chrysomphalus aonidium, Chrysomphalus dictyospermi, Coccus hesperidum, Empoasca spp., Eriosoma lanigerum, Erythroneura spp., Gascardia spp., Laodelphax spp., Lecanium comi, Lepidosaphes spp., Macrosiphus spp., Myzus spp., especially M.persicae; Nephotettix spp., especially N. cincticeps; Nilaparvata spp., especially N. lugens; Paratoria spp., Pemphigus spp., Planococcus spp., Pseudaulacaspis spp., Pseudococcus spp., especially P. Fragilis, P. citriculus and P. comstocki; Psylla spp., especially P. pyri; Pulvinaria aethiopica, Quadraspidiotus spp., Rhopalosiphum spp., Saissetia spp., Scaphoideus spp., Schizaphis spp., Sitobion spp., Trialeurodes vaporariorum, Trioza erytreae and Unaspis citri; 
from the order Hymenoptera, for example Acromyrmex, Atta spp., Cephus spp., Diprion spp., Diprionidae, Gilpinia polytoma, Hoplocampa spp., Lasius spp., Monomorium pharaonis, Neodiprion spp., Solenopsis spp. and Vespa spp.;
from the order Diptera, for example Aedes spp., Antherigona soccata, Bibio hortulanus, Calliphora erythrocephala, Ceratitis spp., Chrysomyia spp., Culex spp., Cuterebra spp., Dacus spp., Drosophila melanogaster, Fannia spp., Gastrophilus spp., Glossina spp., Hypoderma spp., Hyppobosca spp., Liriomyza spp., Lucilia spp., Melanagromyza spp., Musca spp., Oestrus spp., Orseolia spp., Oscinella frit, Pegomya hyoscyami, Phorbia spp., Rhagoletis pomonella, Sciara spp., Stomoxys spp., Tabanus spp., Tannia spp. and Tipula spp.;
from the order Siphonaptera, for example Ceratophyllus spp. and Xenopsylla cheopis; 
from the order Thysanura, for example Lepima saccharina and
from the order Acarina, for example Acarus siro, Aceria sheldoni; Aculus spp., especially A. schlechtendali; Amblyomma spp., Argas spp., Boophilus spp., Brevipalpus spp., especially B. californicus and B. phoenicis; Bryobia praetiosa, Calipitrimerus spp., Chorioptes spp., Dermanyssus gallinae, Eotetranychus App., especially E. carpini and E. orientalis; Eriophyes spp., especially E. vitis; Hyalomma aspp., Ixodea spp., Olygonychus pratensis, Ornithodoros spp., Panonychus pp., especially P. ulmi and P. citri; Phyllocoptruta spp., especially P. oleivora; Polyphagotarsonemus spp., especially P. latus; Psoroptes spp., Rhipicephalus spp., Rhizoglyphus spp., Sarcoptes spp., Tarsonemus spp. and Tetranychus spp., in particular T. urticae, T. cinnabarinus and T. Kanzawai; 
representatives of the class Nematoda;
(1) nematodes selected from the group consisting of root knot nematodes, cyst-forming nematodes, stem eelworms and foliar nematodes;
(2) nematodes selected from the group consisting of Anguina spp.; Aphelenchoides spp.; Ditylenchus spp.; Globodera spp., for example Globodera rostochiensis; Heterodera spp., for example Heterodera avenae, Heterodera glycines, Heterodera schachtii or Heterodera trifolii; Longidorus spp.; Meloidogyne spp., for example Meoidogyne incognita or Meloidogyne javanica; Pratylenchus, for example Pratylenchus neglectans or Pratylenchus penetrans; Radopholus spp., for example Radopholus similis; Trichodorus spp.; Tylenchulus, for example Tylenchulus semipenetrans; and Xiphinema spp.; or
(3) nematodes selected from the group consisting of Heterodera spp., for example Heterodera glycines; and Meloidogyne spp., for example Meloidogyne incognita. 
The method according to the invention allows pests of the abovementioned type to be controlled, i.e. contained or destroyed, which occur, in particular, on transgenic plants, mainly useful plants and ornamentals in agriculture, in horticulture and in forests, or on parts, such as fruits, flowers, foliage, stalks, tubers or roots, of such plants, the protection against these pests in some cases even extending to plant parts which form at a later point in time.
The method according to the invention can be employed advantageously for controlling pests in rice, cereals such as maize or sorghum; in fruit, for example stone fruit, pome fruit and soft fruit such as apples, pears, plums, peaches, almonds, cherries or berries, for example strawberries, raspberries and blackberries; in legumes such as beans, lentils, peas or soya beans; in oil crops such as oilseed rape, mustard, poppies, olives, sunflowers, coconuts, castor-oil plants, cacao or peanuts; in the marrow family such as pumpkins, cucumbers or melons; in fibre plants such as cotton, flax, hemp or jute; in citrus fruit such as oranges, lemons, grapefruit or tangerines; in vegetables such as spinach, lettuce, asparagus, cabbage species, carrots, onions, tomatoes, potatoes, beet or capsicum; in the laurel family such as avocado, Cinnamonium or camphor; or in tobacco, nuts, coffee, egg plants, sugar cane, tea, pepper, grapevines, hops, the banana family, latex plants or omamentals, mainly in maize, rice, cereals, soya beans, tomatoes, cotton, potatoes, sugar beet, rice and mustard; in particular in cotton, rice, soya beans, potatoes and maize.
It has emerged that the method according to the invention is valuable preventatively and/or curatively in the field of pest control even at low use concentrations of the pesticidal composition and that a very favourable biocidal spectrum is achieved thereby. Combined with a favourable compatibility of the composition employed with warm-blooded species, fish and plants, the method according to the invention can be employed against all or individual developmental stages of normally-sensitive, but also of normally-resistant, animal pests such as insects and representatives of the order Acarina, depending on the species of the transgenic crop plant to be protected from attack by pests. The insecticidal and/or acaricidal effect of the method according to the invention may become apparent directly, i.e. in a destruction of the pests which occurs immediately or only after some time has elapsed, for example, during ecdysis, or indirectly, for example as a reduced oviposition and/or hatching rate, the good action corresponding to a destruction rate (mortality) of at least 40 to 50%.
Depending on the intended aims and the prevailing circumstances, the pesticides within the scope of invention , which are known per se, are emulsifiable concentrates, suspension concentrates, directly sprayable or dilutable solutions, spreadable pastes, dilute emulsions, wettable powders, soluble powders, dispersible powders, wettable powders, dusts, granules or encapsulations in polymeric substances which comprise pymetrozine; profenofos; a benzoylurea-derivative or a carbamat-derivative.
The active ingredients are employed in these compositions together with at least one of the auxiliaries conventionally used in art of formulation, such as extenders, for example solvents or solid carriers, or such as surface-active compounds (surfactants).
Formulation auxiliaries which are used are, for example, solid carriers, solvents, stabilizers, xe2x80x9cslow releasexe2x80x9d auxiliaries, colourants and, if appropriate, surface-active substances (surfactants). Suitable carriers and auxiliaries are all those substances which are conventionally used for crop protection products. Suitable auxiliaries such as solvents, solid carriers, surface-active compounds, non-ionic surfactants, cationic surfactants, anionic surfactants and other auxiliaries in the compositions employed according to the invention are, for example, those which have been described in EP-A-736 252.
These compositions for controlling pests can be formulated, for example, as wettable powders, dusts, granules, solutions, emulsifiable concentrates, emulsions, suspension concentrates or aerosols. For example, the compositions are of the type described in EP-A-736 252.
The action of the compositions within the scope of invention which comprise pymetrozine, profenofos, a benzoylurea-derivative or a carbamat-derivative, can be extended substantially and adapted to prevailing circumstances by adding other insecticidally, acaricidally and/or fungicidally active ingredients. Suitable examples of added active ingredients are representatives of the following classes of active ingredients: organo-phosphorous compounds, nitrophenols and derivatives, formamidines, ureas, carbamates, pyrethroids, chlorinated hydrocarbons; especially preferred components in mixtures are, for example, are NI-25, TI-304, Clothiamidin (TI-435), MTI-446, fipronil, pyriproxyfen, thiacloprid, fluxofenime; imidacloprid, thiamethoxam, diafenthiuron, diazinon, disulphoton; furathiocarb, cyromazin, cypermethrin, tau-fluvalinate, tefluthrin or Bacillus thuringiensis products,
As a rule, the compositions within the scope of invention comprise 0.1 to 99%, in particular 0.1 to 95 %, of an active ingredient according to the invention and 1 to 99.9 %, in particular 5 to 99.9 %, ofxe2x80x94at leastxe2x80x94one solid or liquid auxiliary, it being possible, as a rule, for 0 to 25 %, in particular 0.1 to 20 %, of the compositions to be surfactants (% in each case meaning per cent by weight). While concentrated compositions are more preferred as commercial products, the end user will, as a rule, use dilute compositions which have considerably lower concentrations of active ingredient.
The compositions according to the invention may also comprise other solid or liquid auxiliaries, such as stabilisers, for example epoxidized or unepoxidized vegetable oils (for example epoxidized coconut oil, rapeseed oil or soya bean oil), antifoams, for example silicone oil, preservatives, viscosity regulators, binders and/or tackifiers, and also fertilizers or other active ingredients for achieving specific effects, for example, bactericides, fungicides, nematicides, molluscicides or herbicides.
The compositions according to the invention are produced in a known manner, for example prior to mixing with the auxiliary/auxiliaries by grinding, screening and/or compressing the active ingredient, for example to give a particular particle size, and by intimately mixing and/or grinding the active ingredient with the auxiliary/auxiliaries.
The method according to the invention for controlling pests of the abovementioned type is carried out in a manner known per se to those skilled in the art, depending on the intended aims and prevailing circumstances, that is to say by spraying, wetting, atomizing, dusting, brushing on, seed dressing, scattering or pouring of the composition. Typical use concentrations are between 0.1 and 1000 ppm, preferably between 0.1 and 500 ppm of active ingredient. The application rate may vary within wide ranges and depends on the soil constitution, the type of application (foliar application; seed dressing; application in the seed furrow), the transgenic crop plant, the pest to be controlled, the climatic circumstances prevailing in each case, and other factors determined by the type of application, timing of application and target crop. The application rates per hectare are generally 1 to 2000 g of an active ingredient according to the invention per hectare, in particular 10 to 1000 g/ha, preferably 10 to 500 g/ha, especially preferably 10 to 200 g/ha.
A preferred type of application in the field of crop protection within the scope of invention is application to the foliage of the plants (foliar application), it being possible to adapt frequency and rate of application to the risk of infestation with the pest in question. However, the active ingredient may also enter into the plants via the root system (systemic action), by drenching the site of the plants with a liquid composition or by incorporating the active ingredient in solid form into the site of the plants, for example into the soil, for example in the form of granules (soil application). In the case of paddy rice crops, such granules may be metered into the flooded paddy field.
The compositions according to invention are also suitable for protecting propagation material of transgenic plants, for example seed, such as fruits, tubers or kernels, or plant cuttings, from animal pests, in particular insects and representatives of the order Acarina. The propagation material can be treated with the composition prior to application, for example, seed being dressed prior to sowing. The active ingredient may also be applied to seed kernels (coating), either by soaking the kernels in a liquid composition or by coating them with a solid composition. The composition may also be applied to the site of application when applying the propagation material, for example into the seed furrow during sowing. These treatment methods for plant propagation material and the plant propagation material treated thus are a further subject of the invention.